Design, Synthesis and Biological Activity of (20S,21S)-7-Cyclohexyl-21-fluorocamptothecin Carbamates as Potential Antitumor Agents
Design, Synthesis and Biological Activity of (20S,21S)-7-Cyclohexyl-21-fluorocamptothecin Carbamates as Potential Antitumor Agents
复制标题
潜在抗肿瘤药物(20S,21S)-7-环己基-21-氟喜树碱氨基甲酸酯的设计、合成及生物活性
DOI：
10.1002/cbdv.202000068
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发表时间：
2020
影响因子：
2.9
通讯作者：
Miao Zhenyuan
中科院分区：
文献类型：
--
作者：
Ma Haijun;Chen Baobao;Wang Yuan;Wang Chuanhao;Yao Jianzhong;Zhang Wannian;Miao Zhenyuan
(20S,21S)‐7‐Cyclohexyl‐21‐fluorocamptothecin was discovered by a fluorine drug design strategy with potent antitumor activity and increased metabolic stability. In continuous efforts to find novel antitumor agents derived from natural product camptothecin, 20‐carbamates of the active compound (20S,21S)‐7‐cyclohexyl‐21‐fluorocamptothecin have been designed and synthesized. Among them, one compound with the diethylamino group showed greater antiproliferative activity than the other 20‐carbamate derivatives. The following biological activity assays indicated that the above compound is a valuable lead compound with excellent Topo I inhibitory activity and solution stability.
